Designed oligomers of cyanovirin-N show enhanced HIV neutralization

Proc Natl Acad Sci U S A. 2011 Aug 23;108(34):14079-84. doi: 10.1073/pnas.1108777108. Epub 2011 Jul 28.

Abstract

Cyanovirin-N (CV-N) is a small, cyanobacterial lectin that neutralizes many enveloped viruses, including human immunodeficiency virus type I (HIV-1). This antiviral activity is attributed to two homologous carbohydrate binding sites that specifically bind high mannose glycosylation present on envelope glycoproteins such as HIV-1 gp120. We created obligate CV-N oligomers to determine whether increasing the number of binding sites has an effect on viral neutralization. A tandem repeat of two CV-N molecules (CVN(2)) increased HIV-1 neutralization activity by up to 18-fold compared to wild-type CV-N. In addition, the CVN(2) variants showed extensive cross-clade reactivity and were often more potent than broadly neutralizing anti-HIV antibodies. The improvement in activity and broad cross-strain HIV neutralization exhibited by these molecules holds promise for the future therapeutic utility of these and other engineered CV-N variants.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Anti-HIV Agents / chemistry
  • Anti-HIV Agents / immunology
  • Anti-HIV Agents / pharmacology
  • Bacterial Proteins / chemistry*
  • Bacterial Proteins / immunology*
  • Bacterial Proteins / pharmacology
  • Binding Sites
  • Carrier Proteins / chemistry*
  • Carrier Proteins / immunology*
  • Carrier Proteins / pharmacology
  • Crystallography, X-Ray
  • HIV Antibodies / immunology
  • HIV-1 / drug effects
  • HIV-1 / immunology*
  • Models, Molecular
  • Mutant Proteins / chemistry
  • Mutant Proteins / immunology
  • Mutant Proteins / pharmacology
  • Neutralization Tests*
  • Protein Multimerization / drug effects
  • Protein Structure, Quaternary
  • Protein Structure, Tertiary
  • Solutions

Substances

  • Anti-HIV Agents
  • Bacterial Proteins
  • Carrier Proteins
  • HIV Antibodies
  • Mutant Proteins
  • Solutions
  • cyanovirin N

Associated data

  • PDB/3S3Y
  • PDB/3S3Z